Introduction

Question 1

Name the 3 main types of receptor, and give an example for each type

Answer 1

1. Ligand gated ion channels (ionotropic) - eg glycine receptor, PX2
2. Metabotropic receptors - eg GPCRs
3. Kinase Linked Receptors - e.g. RTKs, Cytokine Receptors

Question 2

give 2 reasons why receptors are easy drug targets

Answer 2

1. drugs designed to penetrate membranes have complex chemistries. This is not required for drugs that target receptors, as they do not need to penetrate membranes
2. proteins found inside cells are often ubiquitously expressed, therfore targeting them is more likely to produce off target effects. On the other hand, membrane receptors are selectively expressed, therefore are less likely to produce off target effects.

Question 3

name 6 things that need to be considered when designing new drugs

Answer 3

1. understanding of the disease mechanism
2. to identify receptors that could be targeted
3. consider the potential off target effects and toxicity of the designed drug
4. understand the receptors in terms of structure, function, expression pattern and signalling pathways
5. develop in vitro screens to study drug/receptor interractions
6. develop a disease model to study the effects of the drug.